The synthesis and nicotinic binding activity of (+/-)-epiquinamide and (+/-)-C(1)-epiepiquinamide.
作者： Akira Kanakubo , Diane Gray , Neal Innocent , Susan Wonnacott , Timothy Gallagher
DOI: 10.1016/J.BMCL.2006.05.100
关键词: Curtius rearrangement 、 Biological activity 、 Epibatidine 、 Stereochemistry 、 Ligand binding assay 、 Nicotinic agonist 、 Binding site 、 Chemical synthesis 、 Chemistry 、 Bicyclic molecule
摘要: The synthesis of (+/-)-epiquinamide 1 and (+/-)-C(1)-epiepiquinamide 2 based on the use a Curtius rearrangement to introduce C(1) amino residue is reported. In competition binding assay for [(3)H]epibatidine rat brain membranes neither (+/-)-1 nor (+/-)-2 showed any significant level nicotinic activity.
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